Company: Novartis Ireland Limited.
Legal category: Prescription. High tech. Sport permitted.
Active ingredient: Ruxolitinib (as phosphate) 5mg, 15mg, 20mg.
Description: Round, ovaloid or elongated, curved, white tablets marked NVR on one side and L5, L15 or L20 on reverse, respectively.
Presentation: 56, price available on request.
Indications: Treatment of disease-related splenomegaly or symptoms with primary myelofibrosis, post polycythaemia vera myelofibrosis or post essential thrombocythaemia myelofibrosis.
Pharmacology: Ruxolitinib is a selective inhibitor of the Janus Associated Kinases (JAKs) JAK1 and JAK2. It inhibits JAK-STAT signalling and cell proliferation of cytokine-dependent cellular models of haematological malignancies, as well as of Ba/F3 cells rendered cytokine-independent by expressing the JAK2V617F mutated protein.
Dosage: Adult: Starting dose (administer twice daily): Platelet count, 50,000 – <100,000/mm3, 5mg (titrate cautiously); 100,000 – 200,000/mm3, 15mg; >200,000/mm3, 20mg. Dose modifications: See SPC. Do not increase starting dose within the first 4 weeks of treatment and increase in 2 week intervals thereafter. Maximum 25mg twice daily. Hepatic impairment, severe renal impairment: Reduce dosage by approximately 50%. End-stage renal disease on haemodialysis: Administer post-dialysis and only on day of haemodialysis. Platelet count, 100,000 – 200,000/mm3, single dose of 15mg; >200,000/mm3, single dose of 20mg. See SPC. Elderly: As per adults. Children: Under 18 years, safety and efficacy not established.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy, lactation.
Special precautions: Perform complete blood cell count (including differential) before initiation, every 2-4 weeks until doses are stabilised and as clinically indicated thereafter; neutropenia (temporarily suspend), anaemia (consider dose modification) and thrombocytopenia may occur. Resolve serious infections prior to initiation; carefully monitor for infections (especially herpes zoster). Hepatic impairment; monitor complete blood counts (including differential) at least every 1-2 weeks for the first 6 weeks after initiation and as clinically indicated thereafter once liver function and blood counts have stabilised (titrate to reduce risk of cytopenia). Frequently monitor patients with baseline haemoglobin <10g/dl. Monitor closely for progressive multifocal leukoencephalopathy; if suspected suspend treatment until excluded. Discontinue after 6 months if no reduction in spleen size or improvement in symptoms. Patients with platelet counts <200,000/mm3 at the start of therapy (more likely to develop thrombocytopenia). Peritoneal dialysis or continuous venovenous haemofiltration (no data). Contains lactose. Driving/using machines (dizziness).
Drug interactions: Strong CYP3A4 inhibitors (including boceprevir, lopinavir, mibefradil, posaconazole, telaprevir, telithromycin), dual inhibitors of CYP2C9 and CYP3A4 enzymes. CYP3A4 inducers (including avasimibe, phenobarbital, rifabutin). Moderate CYP3A4 inhibitors. Orally administered CYP3A4 substrates. Drugs transported by P-glycoprotein or breast cancer resistance protein. See appendix I.
Adverse drug reactions: Urinary tract infections, herpes zoster, anaemia, thrombocytopenia, neutropenia, bleeding (including intracranial, gastrointestinal, bruising, epistaxis, post-procedural haemorrhage, haematuria), weight gain, hypercholesterolaemia, dizziness, headache, flatulence, raised alanine aminotransferase, raised aspartate aminotransferase.
Full prescribing information and references available from Novartis Ireland Limited. Telephone: (01) 2601255.
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